1. Field of the Invention
This invention is directed to a new class of organic compounds and is more particularly concerned with 1-piperazino-6-(2-pyridyl)-4H-s-triazolo[4,3-a][1,4]benzodiazepines (II) and a process of production therefor.
The novel compounds II and the process of production therefor can be illustratively represented as follows: ##SPC4##
Wherein R is hydrogen, alkyl of 1 to 3 carbon atoms, inclusive, or .beta.-hydroxyethyl; wherein R.sub.1 is hydrogen or alkyl defined as above; and wherein R.sub.2 and R.sub.3 are hydrogen, alkyl as defined above, fluoro, chloro, bromo, nitro, or trifluoromethyl, and wherein X is chloro or bromo.
The invention further comprises the pharmacologically acceptable acid addition salts of the compounds of formula II.
The more desirable products are of the formula 11A: ##SPC5##
wherein R' is hydrogen, methyl, ethyl, or .beta.-hydroxyethyl; R'.sub.2 is hydrogen, fluoro, chloro, bromo, nitro, or trifluoromethyl, and the pharmacologically acceptable acid addition salts of the compounds of formula IIA.
The most desirable products are of the formula IIB: ##SPC6##
wherein R" is methyl, ethyl, or .beta.-hydroxyethyl; and wherein R".sub.2 is hydrogen, fluoro, chloro, or bromo, and the pharmacologically acceptable acid addition salts thereof.
The process of this application comprises: heating to 100.degree. to 150.degree. C. compound of formula I with an excess of the selected piperazine of the formula: ##SPC7##
Wherein R is defined as hereinabove, for a period of 6 to 24 hours, to obtain the corresponding compound of formula II.